期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 185, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.111833
关键词
Amines; Amides; Antiproliferative activity; Phenatrenes; Mode of action analysis; Naphtho[2,1-b]thiophenes
资金
- Croatian Science Foundation [4379]
- Croatian Government through project Bioprospecting of the Adriatic Sea [KK.01.1.1.01.0002]
- European Union (European Regional Development Fund the Competitiveness and Cohesion Operational Programme) through project Bioprospecting of the Adriatic Sea [KK.01.1.1.01.0002, KK.01.1.1.01]
- University of Rijeka [uniri-biomed-18-133]
- European Regional Development Fund (ERDF)
- European Research Council (ERC) [278212, 770827]
- Serbian Ministry of Education and Science [11144006]
- Slovenian Research Agency (ARRS) [J1-8155]
- Medical Research Council
- Arthritis Research UK
- British Heart Foundation
- Cancer Research UK
- Chief Scientist Office
- Economic and Social Research Council
- Engineering and Physical Sciences Research Council
- National Institute for Health Research
- National Institute for Social Care and Health Research
- Wellcome Trust [MR/K006584/1]
Herein we present and describe the design and synthesis of novel phenantrene derivatives substituted with either amino or amido side chains and their biological activity. Antiproliferative activities were assessed in vitro on a panel of human cancer cell lines. Tested compounds showed moderate activity against cancer cells in comparison with 5-fluorouracile. Among all tested compounds, some compounds substituted with cyano groups showed a pronounced and selective activity in the nanomolar range of inhibitory concentrations against HeLa and HepG2. The strongest selective activity against Hel-a cells was observed for acrylonitriles 8 and 11 and their cyclic analogues 15 and 17 substituted with two cyano groups with a corresponding IC50 = 033, 0.21, 0.65 and 0.45 mu M, respectively. Compounds 11 showed the most pronounced selectivity being almost non cytotoxic to normal fibroblasts. Additionally, mode of biological action analysis was performed in silica and in vitro by Western blot analysis of HIF-1-alpha, relative expression for compounds 8 and 11. (C) 2019 Elsevier Masson SAS. All rights reserved.
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